GSK 2332255B is a potent, and selective inhibitor of TRPC3/6 channels with IC50 of 3 nM/21 nM, respectively. It dispalys >100-fold selectivity over other calcium-permeable channels. It has 100-fold greater potency for TRPC3 compared with Pyr3. GSK 2332255B (dose-dependent) blocks cell hypertrophy signaling triggered by angiotensin II or endothelin-1 in HEK293T cells as well as in neonatal and adult cardiac myocytes.
GSK2332255B is a potent, selective TRPC3 and TRPC6 antagonist with IC50s of 5 nM and 4 nM for rat TRPC3 and rat TRPC6. GSK2332255B shows ≥100-fold selectivity for TRPC3/6 over other calcium-permeable channels[1].
